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Pharmacology II > Pituitary and Gonadal Hormones II > Flashcards

Pituitary and Gonadal Hormones II Flashcards

1
Q

What is inhibited until puberty?

Which neuron system is involved in this inhibition?

A

GnRH release

Kisspeptin, Neurokinase B and Dynorphin

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2
Q

Early menstrual changes are followed by what? (2)

A

Periodic cyclical bleeding

Secretion of GnRH, gonadotropins and ovarian hormones

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3
Q

Cessation of menstruation cycle :
Can still make ______
symptoms? (3)

A

Estrogen
Hot flashes
CV events
Osteoporosis

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4
Q

Steps to the menstrual cycle?

No pregnancy?

A
  1. FSH stimulates multiple follicles
  2. Dominant follicle grows
  3. LH/FSH surge, follicle rupture, ovulation and corpus hemorrhagicum formation
  4. Luteinized granulosa and thecal cells form corpus luteum (progesterone and estrogen)
    No pregnancy : CL degenerates, endometrial sloughing and menstruation
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5
Q

Disturbances in ovarian function? (5)

A

Amenorrhea (absence of menstrual cycle)
Anovulation (absence of ovulation)
Tumors in ovary, pituitary gland and uterus
Prolactinomas (inhibition of GnRH release)
Hormonal disturbances : Tumors of adrenal gland

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6
Q

Three forms of estrogen?

Major form?

A

Estradiol (E2)
Estrone (E1)
Estriol (E3)
Major : Estradiol

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7
Q

Estrogen mimetic compounds? (2)

A 
Flavonoids
Plastic manufacturing (bisphenols, lkylphenols, phthalate phenols)
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8
Q

Biosynthesis of estrogens and testosterone? (3)

A
  1. Pregnenolone is the precursor of progesterone, dehydropiandrosterone and androstenedione
  2. Aromatase converts androstenedione and testosterone into estrone (E1) and estradiol (E2)
  3. E1 and E3 are formed in the liver from E2 and in peripheral tissues from androstenedione and androgens.
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9
Q

Estrogen in circulation binds to what? active or inactive?

A

Sex hormone-binding globulin (SHBG)

Not active

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10
Q

When estrogen enters the nucleus, it binds to _____ receptors.
Two receptor isoforms in the nucleus? Roles?

A

estrogen
ERalpha: growth promoting
ERbeta: antigrowth effects

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11
Q

Once estrogen binds to estrogen receptor in the nucleus, this forms _____ that bind to _______ and ________

A

Dimers

Estrogen response elements (ERE) and CoA/CoR (transcription and protein synthesis)

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12
Q

Non-genomic actions of estrogen? (2)

A

Binds to cell surface receptors

Activates different signal transduction pathways

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13
Q

Physiologic effects of estrogen:

Normal or abnormal sexual maturation?

A

Normal

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14
Q

Physiologic effects of estrogen:

Increases levels of _____ factors, decreases _______ ______ and which disease?

A

Clotting factors
Platelet adhesiveness
Atherosclerosis

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15
Q

Physiologic effects of estrogen:

liver metabolism?

A

increases levels of hormone binding globulins, transferrin and fibrinogen

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16
Q

Physiologic effects of estrogen: effects on cholesterol and TG?

A

Increases plasma HDL and TG

Lowers LDL and cholesterol

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17
Q

2 clinical uses of synthetic estrogens?

A

Primary hypogonadism

Hormone replacement therapy (HRT)

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18
Q

What is primary hypogonadism and how is it treated?

A

Ovarian developmental defects, surgical oophorectomy, premature menopause
Treatment : ethinyl estradiol, conjugated or esterified estrogens (equilin)

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19
Q

Hormone replacement therapy is used on which women?
It has beneficial effects on circulating ____ and ________
WHI found increased risks for what? (2)

A

postmenopausal women
Circulation lipids and lipoproteins
CV problems and breast cancer

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20
Q

Adverse effects and contraindications of estrogen therapies? (3)

A

Uterine and vaginal bleeding
Breast cancer risk
Should not be used in estrogen dependent cancer, liver disease, thromboembolic disease

21
Q

What is the major progestin?
It is synthesized where? (4)
MOA similar to ___________

A

Progesterone
Ovary, testis, adrenal cortex, placenta
Estrogen

22
Q

Progesterone :

promotes ____ and ______ deposition, increases ________ response to glucose

A

fat and glycogen

insulin

23
Q

Progesterone :

_________ effects on the brain

A

hypnotic

24
Q

Progesterone competes with _________ binding to _______ receptors in renal tubule and promotes renal ____ excretion

A

aldosterone
mineralocorticoid
Na+

25
Q

Synthetic progestins have an increased half-life of how many days?

A

1-3

26
Q

Second generation synthetic progestins are ____ compounds.

Example?

A

21-C

Medroxyprogesterone

27
Q

Third generation synthetic progestins are ___ steroids and include ____ _________.
example?

A

19-nor, 13-ethyl steroids
Oral contraceptives
Norgestimate

28
Q

2 clinical applications of synthetic progestins?

A

Hormone replacement therapy

Prolonged ovarian suppression

29
Q

Hormone replacement therapy with synthetic progestins are used in which women?
Progestins are used in combination with ______

A

postmenopausal

estrogen

30
Q

Synthetic progestins:
prolonged ovarian suppression is used for which diseases? (2)
Does it activate or inhibit gonadotropin release?

A

Dysmenorrhea
Endometriosis
Inhibit

31
Q

Drugs/devices that prevent contraception? (4)

A

Spermicides
Barrier methods
Intrauterine devices
Oral, injectable transdermal

32
Q

Two combinations of oral preparations of hormonal contraceptions?

A

1) Estrogen and progestin combinations

2) Progestins alone

33
Q

2 combination preparation forms of hormonal preparations? Examples?

A

Monophasic form : Yasmin

Multiphasic form : Natazia

34
Q

Natazia:

the amount of _______ valerate is stepped down while the amount of _______ is stepped up

A

estradiol

progestin

35
Q

Natazia : roles? (2)

A

Feedback inhibition of gonadotropin release

Inhibition of ovulation

36
Q

Birth control path is a combination of which two hormones?

A

Norelgestromin

Ethinyl estradiol

37
Q

Two examples of Emergency Contraception? what do they involve?

A

Plan B One-Step : single dose of levonogestrel (Progestin)

Plan B Next Choice : two doses of levonogestrel

38
Q

What causes a decrease in efficacy of oral contraceptives? (2)

A

antimicrobial agents

rifampicin

39
Q

What type of drugs are Selective Estrogen Receptor Modulators (SERMs)?

A

Competitive partial agonist inhibitors of estradiol at ER

40
Q

Where are SERMs agonists? (4)

Where are they antagonists? (2)

A

Liver, CV, bone and uterus

Breast and Brain

41
Q

Two examples of SERMs? Role?

A

Tamoxifen
Clomiphene
Agonists: They act like estrogen and eliminate estrogen function

42
Q

How is tamoxifen metabolized into a more potent SERM?

A

CYP2D6 metabolizes tamoxifen into endoxifen

43
Q

2 progesterone inhibitors?

A

Mifepristone

Danazol

44
Q

Role of mifepristone?

A

Binds to progesterone and glucocorticoid receptors and inhibits activities of ligands

45
Q

Danazol:
Weak binding to which receptors? (3)
Inhibits what? (3)

A

Weak binding to progesterone, androgen and glucocorticoid receptors
Inhibits midcycle LH/FSH surge
Inhibits enzymes including P450C17
Inhibits conversion of progesterone into androstenedione and testosterone

46
Q

Nafarelin is a ______ analog and inhibits what?

A

GnRH

Ovarian function

47
Q

Anastrozole inhibits _______

A

aromatase

48
Q

Fulvestrant is a ____ antagonist.

It inhibits the dimerization of what?

A

ER

Dimerization of ER and DNA binding

Pharmacology II (21 decks)

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